KR20160115936A - 알츠하이머병의 치료를 위한 bace1 저해제로서의 2-아미노-3,5,5-트리플루오로-3,4,5,6-테트라하이드로피리딘 - Google Patents

알츠하이머병의 치료를 위한 bace1 저해제로서의 2-아미노-3,5,5-트리플루오로-3,4,5,6-테트라하이드로피리딘 Download PDF

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KR20160115936A
KR20160115936A KR1020167021930A KR20167021930A KR20160115936A KR 20160115936 A KR20160115936 A KR 20160115936A KR 1020167021930 A KR1020167021930 A KR 1020167021930A KR 20167021930 A KR20167021930 A KR 20167021930A KR 20160115936 A KR20160115936 A KR 20160115936A
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trifluoro
dimethyl
amino
fluorophenyl
tetrahydronaphthalen
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카르스텐 율
마우로 마리고
레나 타그모세
토마스 옌센
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하. 룬드벡 아크티에셀스카브
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D227/00—Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00
    • C07D227/02—Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00 with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D227/06—Heterocyclic compounds containing rings having one nitrogen atom as the only ring hetero atom, according to more than one of groups C07D203/00 - C07D225/00 with only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D227/10—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020167021930A 2014-02-19 2015-02-17 알츠하이머병의 치료를 위한 bace1 저해제로서의 2-아미노-3,5,5-트리플루오로-3,4,5,6-테트라하이드로피리딘 Withdrawn KR20160115936A (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
DKPA201400086 2014-02-19
DKPA201400086 2014-02-19
DKPA201400349 2014-07-01
DKPA201400349 2014-07-01
PCT/EP2015/053327 WO2015124576A1 (en) 2014-02-19 2015-02-17 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease

Publications (1)

Publication Number Publication Date
KR20160115936A true KR20160115936A (ko) 2016-10-06

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KR1020167021930A Withdrawn KR20160115936A (ko) 2014-02-19 2015-02-17 알츠하이머병의 치료를 위한 bace1 저해제로서의 2-아미노-3,5,5-트리플루오로-3,4,5,6-테트라하이드로피리딘

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US (2) US20170066741A1 (https=)
EP (1) EP3107897A1 (https=)
JP (1) JP6483146B2 (https=)
KR (1) KR20160115936A (https=)
CN (1) CN106029639B (https=)
AP (1) AP2016009370A0 (https=)
AR (1) AR099489A1 (https=)
AU (1) AU2015220873A1 (https=)
CA (1) CA2940028A1 (https=)
CL (1) CL2016002072A1 (https=)
CR (1) CR20160352A (https=)
DO (1) DOP2016000194A (https=)
EA (1) EA031132B1 (https=)
EC (1) ECSP16072941A (https=)
GE (2) GEAP201814248A (https=)
IL (1) IL246875A0 (https=)
MA (1) MA39225A1 (https=)
MX (1) MX2016010777A (https=)
PE (1) PE20161225A1 (https=)
PH (1) PH12016501600A1 (https=)
RU (1) RU2016133626A (https=)
SG (1) SG11201606812WA (https=)
TW (1) TW201609700A (https=)
UA (1) UA117695C2 (https=)
WO (1) WO2015124576A1 (https=)

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KR20190123584A (ko) 2018-04-24 2019-11-01 삼성에스디에스 주식회사 부채널 공격에 안전한 연산 장치 및 방법

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JO3458B1 (ar) 2014-11-10 2020-07-05 H Lundbeck As 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1
MA40941A (fr) * 2014-11-10 2017-09-19 H Lundbeck As 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1
CR20170187A (es) * 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer
JO3627B1 (ar) 2015-04-30 2020-08-27 H Lundbeck As إيميدازو بيرازينونات على هيئة مثبطات pde1
TW201717948A (zh) * 2015-08-10 2017-06-01 Ｈ 朗德貝克公司 包括給予２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶的聯合治療
AU2016305275A1 (en) * 2015-08-12 2018-02-08 H. Lundbeck A/S 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridins as bace1 inhibitors
CA2997947A1 (en) 2015-09-09 2017-03-16 The Trustees Of Columbia University In The City Of New York Reduction of er-mam-localized app-c99 and methods of treating alzheimer's disease
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RU2019109039A (ru) 2016-10-28 2020-11-30 Х. Лундбекк А/С Комбинированные средства для лечения, предусматривающего введение имидазопиразинонов, предназначенные для лечения психических и/или когнитивных расстройств
TW201829394A (zh) 2016-12-21 2018-08-16 丹麥商Ｈ 朗德貝克公司 作為ｂａｃｅ１抑制劑之６-胺基-５-氟-５-（氟甲基）-２，３，４，５-四氫吡啶-２-基-苯基-５-（甲氧基-ｄ）-吡-２-甲醯胺及其氟化衍生物
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WO2019071147A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. INHIBITORS OF KINASE P38 REDUCING EXPRESSION OF DUX4 GENE AND DOWNSTREAM GENES FOR THE TREATMENT OF FSHD
AR113926A1 (es) 2017-12-14 2020-07-01 H Lundbeck As Derivados de 1h-pirazolo[4,3-b]piridinas
MX2020006174A (es) 2017-12-14 2022-09-27 H Lundbeck As Tratamientos de combinación que comprenden la administración de 1h-pirazol[4,3-b]piridinas.
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KR20190121995A (ko) 2018-04-19 2019-10-29 삼성에스디에스 주식회사 부채널 공격에 안전한 연산 장치 및 방법
KR20190123584A (ko) 2018-04-24 2019-11-01 삼성에스디에스 주식회사 부채널 공격에 안전한 연산 장치 및 방법

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IL246875A0 (en) 2016-08-31
AP2016009370A0 (en) 2016-08-31
UA117695C2 (uk) 2018-09-10
RU2016133626A3 (https=) 2018-09-25
GEAP201814248A (en) 2018-04-10
EA201691447A1 (ru) 2016-12-30
GEP20186892B (en) 2018-09-10
ECSP16072941A (es) 2017-02-24
DOP2016000194A (es) 2016-09-30
JP2017506237A (ja) 2017-03-02
US20170066741A1 (en) 2017-03-09
WO2015124576A1 (en) 2015-08-27
TW201609700A (zh) 2016-03-16
PH12016501600A1 (en) 2017-02-06
MX2016010777A (es) 2016-10-26
RU2016133626A (ru) 2018-03-20
MA39225A1 (fr) 2017-04-28
AU2015220873A1 (en) 2016-08-11
EP3107897A1 (en) 2016-12-28
CL2016002072A1 (es) 2017-01-20
CN106029639B (zh) 2019-01-08
AR099489A1 (es) 2016-07-27
EA031132B1 (ru) 2018-11-30
CN106029639A (zh) 2016-10-12
US9353084B2 (en) 2016-05-31
US20150232449A1 (en) 2015-08-20
CA2940028A1 (en) 2015-08-27
SG11201606812WA (en) 2016-09-29
PE20161225A1 (es) 2016-12-04
JP6483146B2 (ja) 2019-03-13
CR20160352A (es) 2016-10-20

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